Global Patent Index - EP 0749966 A4

EP 0749966 A4 19970702 - 5-HT 3 RECEPTOR AGONIST, NOVEL THIAZOLE DERIVATIVE, AND INTERMEDIATE THEREFOR

Title (en)

5-HT 3 RECEPTOR AGONIST, NOVEL THIAZOLE DERIVATIVE, AND INTERMEDIATE THEREFOR

Title (de)

5-HT 3-REZEPTOR AGONISTEN, NEUE THIAZOL-DERIVATE UND ZWISCHENPRODUKTE

Title (fr)

AGONISTE DE RECEPTEUR 5-HT 3, NOUVEAU DERIVE DE THIAZOLE ET INTERMEDIAIRE DESTINE A SON OBTENTION

Publication

EP 0749966 A4 19970702 (EN)

Application

EP 95910774 A 19950309

Priority

  • JP 9500385 W 19950309
  • JP 6782294 A 19940311

Abstract (en)

[origin: EP0749966A1] A 5-HT3 receptor agonist containing a thiazole derivative represented by general formula (I) as the effective ingredient; a specified compound useful as a 5-HT3 receptor agonist; and a specified thioamide derivative useful as an intermediate therefor. <CHEM> wherein each symbol represents the following meaning: Ring A: the following ring which may be substituted by one or more substituents selected from the group consisting of a halogen atom, a lower alkyl group and a lower alkoxyl group: 1) a benzene ring, or 2) a 5-membered or 6-membered unsaturated heterocyclic ring having one or two hetero atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, L1 and L2: one of them represents a single bond, and the other one represents non-existence, or an alkylene group having 1 to 4 carbon atoms or an alkenylene group having 2 to 5 carbon atoms, R: a group represented by one of the following formulae: <CHEM> L<3>: a lower alkylene group, L<4>: a single bond or a lower alkylene group, R<1> and R<2>: the same or different and individually a hydrogen atom, a lower alkyl group or an amino-protecting group, R<3>: a hydrogen atom, a lower alkyl group, an oxo group or a protected or unprotected amino group, R<4>: non-existence or a hydrogen atom, a lower alkyl group, an aralkyl group or an amino-protecting group, Ring B: the following monocyclic or bicyclic ring which may contain an oxygen atom: 1) a nitrogen-containing saturated heterocyclic ring having 4 to 16 ring-forming atoms, or 2) a nitrogen-containing heterocyclic ring having one unsaturated bond and 4 to 16 ring-forming atoms, and Ring D: a saturated carbon ring having 4 to 8 ring-forming atoms, in

IPC 1-7

C07D 277/28; C07D 277/60; C07D 277/84; C07D 417/04; C07D 417/06; C07D 417/14; C07D 513/04; A61K 31/425; A61K 31/435; A61K 31/445; A61K 31/535

IPC 8 full level

C07D 277/28 (2006.01); C07D 277/60 (2006.01); C07D 417/04 (2006.01); C07D 417/06 (2006.01); C07D 417/14 (2006.01); C07D 471/04 (2006.01); C07D 471/08 (2006.01); C07D 487/04 (2006.01); C07D 487/08 (2006.01); C07D 513/04 (2006.01); C07D 519/00 (2006.01)

CPC (source: EP KR US)

C07D 277/60 (2013.01 - EP KR US); C07D 417/04 (2013.01 - EP KR US); C07D 417/06 (2013.01 - EP KR US); C07D 417/14 (2013.01 - EP KR US); C07D 471/04 (2013.01 - EP KR US); C07D 471/08 (2013.01 - EP KR US); C07D 487/04 (2013.01 - EP KR US); C07D 487/08 (2013.01 - EP KR US); C07D 513/04 (2013.01 - EP KR US); Y02P 20/55 (2015.11 - EP US)

Citation (search report)

  • [X] JP H05345772 A 19931227 - FUJISAWA PHARMACEUTICAL CO
  • [E] JP H0770136 A 19950314 - YAMANOUCHI PHARMA CO LTD
  • [E] EP 0666263 A1 19950809 - YAMANOUCHI PHARMA CO LTD [JP] & WO 9406791 A1 19940331 - YAMANOUCHI PHARMA CO LTD [JP], et al
  • [E] WO 9524406 A1 19950914 - YAMANOUCHI PHARMA CO LTD [JP], et al
  • [A] DE 2717415 A1 19771110 - LILLY INDUSTRIES LTD
  • [A] EP 0397364 A1 19901114 - PFIZER [US]
  • [A] EP 0555480 A1 19930818 - YAMANOUCHI PHARMA CO LTD [JP] & WO 9207849 A1 19920514 - YAMANOUCHI PHARMA CO LTD [JP]
  • [PX] PERRONE R. ET AL.: "Conformationally restricted thiazole derivatives as novel class of 5-HT3 receptor ligands", IL FARMACO, vol. 50, no. 2, February 1995 (1995-02-01), pages 77 - 82, XP000605205
  • [A] BROWN D.J. ET AL.: "Unfused heterobicycles as amplifiers of phleomycin. III. Thiazolylpyridines and Bipyrimidines with strongly basic side chains", AUSTRALIAN JOURNAL OF CHEMISTRY, vol. 34, no. 11, November 1981 (1981-11-01), pages 2423 - 2429, XP000653389
  • [A] NAGEL A.A. ET AL.: "Aromatic thiazole derivatives: Structurally novel and selective serotonin-3 receptor antagonists", JOURNAL OF MEDICINAL CHEMISTRY, vol. 33, no. 1, January 1990 (1990-01-01), pages 13 - 16, XP000652147
  • [PA] AZIMOV V.A. ET AL.: "Synthesis of functionally substituted derivatives of thiazolo[4,5-f]quinoline, pyridazino[3,4-f]quinoline and 5-hydroxyquinoline based on 3-cyano-6-bromo-1,2,5,6,7,8-hexahydroquinoline-2,5-dione", PHARMACEUTICAL CHEMISTRY JOURNAL, vol. 28, no. 8, 9 August 1994 (1994-08-09), pages 586 - 588, XP000651748
  • See also references of WO 9524399A1

Designated contracting state (EPC)

AT BE CH DE DK ES FR GB GR IE IT LI LU NL PT SE

DOCDB simple family (publication)

EP 0749966 A1 19961227; EP 0749966 A4 19970702; AU 1862295 A 19950925; AU 686340 B2 19980205; CA 2184685 A1 19950914; CN 1143364 A 19970219; KR 970701705 A 19970412; MX 9603998 A 19971231; NZ 281718 A 19970822; US 5834499 A 19981110; WO 9524399 A1 19950914

DOCDB simple family (application)

EP 95910774 A 19950309; AU 1862295 A 19950309; CA 2184685 A 19950309; CN 95192012 A 19950309; JP 9500385 W 19950309; KR 19960705029 A 19960911; MX 9603998 A 19950309; NZ 28171895 A 19950309; US 70042896 A 19960826